AT7867 as a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A. This ATP-competitive small molecule potently inhibits both AKT and p70S6K activity at the cellular level, as measured by inhibition of GSK3β and S6 ribosomal protein phosphorylation, and also causes growth inhibition in a range of human cancer cell lines as a single agent.
| Cell Experiment | |
|---|---|
| Cell lines | PTEN-negative U87MG human glioblastoma cells |
| Preparation method | Alamar Blue Cell Proliferation Assay. Cells were plated in 96-well microplates at 5000 cells per well in medium supplemented with 10% FBS, and grown for 24 hours before treatment with AT7867. Inhibitor or vehicle control was added to the cells for 72 hours. Following this, Alamar Blue solution (BioSource, Nivelle Belgium) was added as stated in the manufacturer's instructions. The IC50 value for each inhibitor was calculated in GraphPad Prism (San Diego, USA) using non-linear regression analysis and a sigmoidal dose-response (variable slope) equation. |
| Concentrations | 0~100 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | athymic BALB/c mice bearing MES-SA and U87MG human glioblastoma xenograft tumors |
| Formulation | 10% DMSO, 90% saline |
| Dosages | 20mg/kg or 90mg/kg once every 3 days |
| Administration | p.o. |
| Molecular Weight | 337.85 |
| Formula | C20H20ClN3 |
| CAS Number | 857531-00-1 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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